Synthesis, in vitro and in vivo anti-Trypanosoma cruzi and toxicological activities of nitroaromatic Schiff bases

Publication date: December 2018Source: Biomedicine & Pharmacotherapy, Volume 108Author(s): Tamires Cunha Almeida, Luis Henrique Gonzaga Ribeiro, Luzia Braga Ferreira dos Santos, Cleiton Moreira da Silva, Renata Tupinambá Branquinho, Marta de Lana, Fernanda Ramos Gadelha, Ângelo de FátimaAbstractChagas disease is a major health problem not only in Latin America but also in Europe and North America due to the spread of this disease into nonendemic areas. In terms of global burden, this major tropical infection is considered to be one of the most neglected diseases, and there are currently only two available chemotherapies: benznidazole and nifurtimox. Unfortunately, although these chemotherapies are beneficial in the acute phase of the disease, benznidazole and nifurtimox lead to significant side effects, including hepatitis and neurotoxicity. Therefore, the search for and development of more effective, safe and inexpensive anti-Trypanosoma cruzi drugs are required. In this work, a series of 10 nitroaromatic Schiff bases bearing different (nitro) aromatic rings-was synthesized. Subsequently, the in vitro and in vivo anti-T. cruzi activities of the Schiff bases were investigated, as well as the in vivo toxicity and the biological effects. The basic structure of the most promising in vivo Schiff base, 10 would be useful in the synthesis of new compounds for Chagas disease treatment.Graphical abstract

Source: Biomedicine and Pharmacotherapy - October 12, 2018 Category: Drugs & Pharmacology Source Type: research